| Description | BAY-1816032 is a potent and orally available inhibitor of bidding uninhibited by benzimidazoles 1 ( BUB1) kinase (IC50: 7 nM). |
| In vitro | 在分子机制层面，BAY-1816032有效阻断了nocodazole所诱导的HeLa细胞中BUB1的主要靶蛋白组蛋白H2A的Thr-120磷酸化（IC50: 29 nM），诱导滞留染色体和有丝分裂延迟。在与低浓度paclitaxel联合使用时，持续观察到染色体滞后和分裂错误。单一化合物BAY-1816032对多种肿瘤细胞系的增殖具有抑制作用，IC50值为1.4 μM。在几乎所有评估的细胞线中，BAY-1816032与paclitaxel或docetaxel表现出协同效应或增效作用。 |
| In vivo | 在肿瘤异种移植模型研究中，BAY 1816032作为单药口服时对肿瘤生长的抑制作用较为有限，但与Paclitaxel 或Docetaxel 联合使用时肿瘤体积缩减。 |
| Target activity | BUB1 kinase:7 nM |
| molecular weight | 534.51 |
| Molecular formula | C27H24F2N6O4 |
| CAS | 1891087-61-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | H2O: < 0.1 mg/mL (insoluble) DMSO: 15 mg/mL (28.06 mM), Sonication and heating are recommended. |
| References | 1. Siemeister G, et al. BAY 1816032, a novel BUB1 kinase inhibitor with potent antitumor activity [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2017; 2017 Apr 1-5; Ishington, DC. Philadelphia (PA): AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 287. doi:10.1158/1538-7445.AM2017-287 |